Reducing dependence on tobacco

ABSTRACT

Dependence on tobacco is reduced by administration to a person dependent thereon of an effective amount of an extract of Avena plants.

United States atent 11 1 1111 3,862,317 Lal Anand Jan. 21, 1975 [54]REDUCING DEPENDENCE ON TOBACCO 2,600,700 6/1952 Smith 424/255 [76]Inventor: Chaman Lal Anand, 47 Clarendon TH A St., Glasgow G20 '7QP,Scotland 0 ER PUBLIC TIONS R. Wren, Potters Cyclopaedia of BotanicalDrugs & [22] Flled' 1972 preparations, (1950), p. 252, published byPotter & [21] Appl. No.1 217,960 Clark, London, England.

[30] Foreign Application Priority Data Primary Examiner-Stanley J.Friedman Jan. 16, 1971 Great Britain 2231/71 y, g t, r m-Conn lly andHutz [52] U.S. Cl. 424/195 [51] Int. Cl A6lk 27/00 ABSTRACT [58] Fieldof Search 424/195 Dependence on tobacco is reduced y administration I561 References Cited to a person dependent thereon of an effectiveamount of an extract of Avena plants. UNITED STATES PATENTS 2,357,7569/1944 Musher 424/195 10 Claims, N0 Drawings REDUCING DEPENDENCE ONTOBACCO THIS INVENTION relates to reducing dependence on tobacco.

Tobacco is the fermented leaves of a plant of the genus Nicotiana,especially N. tabacum. As is well known, tobacco may be consumed bychewing or as snuff, but is more usually smoked. In recent years it hasbeen generally recognised that tobacco consumption has undesirablelong-termeffects. Lung cancer, in particular, has been shown to beassociated in a statistically very significant way with heavy smoking,especially of cigarettes. Other undesirable long-tern effects have beennoted.

Unfortunately when a person has become habituated to tobacco, he (orshe) generally finds it very difficult to break the habit, and attemptsto do so are often attended by severe mental, and even physical, stress.Existing methods of reducing dependence on tabacco have not proved veryeffective.

When I was in India in 1967, I came across a medically unqualifiedpractitioner of the ancient Ayurvedic medicine who had successfully useda decoction of Avena sativa to cure the opium habit.

When I myself used this treatment but with a tincture rather than adecoction (which I found to be effective in a substantial proportion ofcases) at the Susheela Mehra Memorial Hospital, Jullundur City, Punjab,India, I observed that some of the treated patients lost their cravingfor cigarettes.

I therefore carried out the following trial using a 90% ethyl alcoholicextract of Avena sativa, the preparation of which is described in moredetail below.

Twenty-six cigarette smokers including healthy volunteers and chronicpatients in the chest wards of Ruchill Hospital, Glasgow, Scotland,including tuberculous patients, participated in the trial. The totalduration of their smoking and the average number of cigarettes smokedper day in the preceding 6 months were recorded. They were told that adrug was being tested which might affect their smoking, andthat theywere not to make any conscious effort to alter their smoking during thetrial. Each patient kept a daily record of cigaretts smoked, commentingon any changes in the craving for cigarettes. By random allocation, 13patients received the drug and the others received placebo for 28 days.The alcoholic extract (1 ml.) was diluted to ml. and each oral dose was5 ml. of this dilution given 4 times a day. No psychotherapy was used.No patients were taking any other drugs which could affect smoking. Thepatients in both groups were comparable in age, sex and smoking history.The results of the trial are given in Table I.

TABLE I Number of Cigarettes Smoked During Trial Group 1 (drug) Group 2(placebo) TABLE l-Continued Number of Cigarettes Smoked During TrialGroup 1 (drug) Group 2 (placebo) Cigarettes Cigarettes CigarettesCigarettes per day per day per day per day before trial after trialbefore trial after trial 25 7 l5 14 l0. l0 9 20 I0 8 8 Av. l9.5 5.7 l6.516.7

, Group 1 before (mean 19.5 i 2.0 s.e.) is not statistically separablefrom-Group 2 before (mean 16.5 i 1.7 s.e.)', 1.33, 0.30 P 0.20. Group 1before is significantly different from Group 1 after (mean 5.7 i 2.0s.e.); t= 5.21, P 0.001. Group 2 before is not different from Group 2after. (mean 16.9 :1.4 s.e.); z 0.180, 0.90 P 0.80. The mean differencesbetween the groups due to treatment (Group 1 before Group 1 after) and(Group 2 before Group 2 after) are naturally equally significant; t=5.73, P 0.001. All these calculations are based on Students t test.

In the drug group various degrees of loss of craving for cigarettes werereported. The drug seems to reduce the number of cigarettes smoked perday, along with diminished craving for smoking. Moreover, the reductionin smoking seems to continue even 2 months after the termination of thedrug.

The present invention therefore provides a method of reducing dependenceon tobacco which comprises administering to a person dependent thereonan extract of part or all of an Avena plant, especially A. saliva, thecultivated oat. Other species of Avena, e.g. A. fatua, A. steritis, andA. strigosa, can also be used.

I prefer to use the whole of the mature green plant and to extract itwith an appropriate solvent, e.g. water, ethyl alcohol, acetone, achlorinated hydrocarbon such as chloroform, diethyl ether, or hexane.Mixtures of such solvents, especially aqueous ethyl alcohol, can also beused.

The extraction is conveniently carried out at ambient temperature, e.g.l025C., though higher temperatures which do not adversely affect theextract, e.g. up to 50C., can also be used. The period of extraction canbe from a few hours to several, e.g. 2 to 3 days. The plant should becrushed or comminuted before it is mixed with the solvent. From 1 to 10,preferably about 2 to 4, parts by volume of solvent are used per part byweight of the plant. After the extraction, the plant remains may beremoved by filtration or other convenient means.

When a physiologically tolerated solvent is used, the extract soproduced may be used as it is, or after dilution with the same oranother such solvent miscible therewith, e.g. water. However, when aphysiologically unacceptable solvent is used, it must be removed, e.g.by evaporation at low pressure. The residue of the extract which thenremains may be used as such or after Name Aerosil." After allowing thesolvent to evaporate, the material with the extract from the Avena plantabsorbed or adsorbed thereon may be formulated into a capsule or tabletby conventional means, using conventional, pharmaceutically acceptablecarrier materials.

The invention is illustrated in the following Examples.

EXAMPLE 1 A quantity of healthy, fresh, whole Avena saliva plant,collected just before harvest, is extracted with parts by volume of 90%ethyl alcohol water) to 1.5 parts by weight of crushed plant i.e. 5litres of 90% ethyl alcohol to 1.5 kg. of plant. The mixture is kept atroom temperature for 72 hours with frequent agitation and then filteredto yield a clear, ambercoloured liquid. For administration to cigarettesmokers, 1 ml. of the extract is diluted to 5 ml. with water andadministered four times a day. Flavouring and preservatives may beadded, as desired.

EXAMPLE 2 The liquid extract obtained by the procedure of Example l iscontacted with a quantity of a silica powder of particle size 3 to mp.,sold under the Trade Name Aerosil, in the proportion of 1 ml. of extractto l g. of silica, whereby the substance or substances present in theextract and derived from the Avena saliva plant is absorbed by oradsorbed on the silica. The solvent is allowed to evaporate to yield afree-flowing powder which is then mixed with the ingredients shown inthe following formula:

mg. silica, containing substance(s) extracted from Avena plant 1,000lactose 300 microcrystalline cellulose 250 magnesium stearate 50 1,600

This mixture is then compressed to form a tablet suitable for oraladministration.

EXAMPLE 3 A silica powder, containing the substance or substancesextracted from the Avena plant, is obtained by the procedure of Example2 and blended with 10% by weight of lactose, 2% by weight of starch and1% by weight of magnesium stearate. This mixture is compressed intoslugs and the slugs are inserted into hard gelatin capsules of suitablesize for oral administration.

EXAMPLE 4 The liquid extract obtained in Example 1 is used to filldropper bottles of suitable size, e.g. 100 ml., which are then used toadminister a measured dose of 1 ml. of the liquid, delivered by adropper of 1 ml. capacity. The measured dose may be delivered into aglass of water as diluent, or onto a suitable carrier, e.g. a sugarlump.

EXAMPLE 5 The liquid extract obtained by the procedure of Example l isevaporated in vacuo to yield 2% by weight of a gummy residue, which istriturated with diethyl ether and the latter solvent is removed byvacuum evaporation. The solid residue is then suspended in watertogether with sodium carboxymethyl cellulose (5% by weight, based on thewater content) and flavouring, to give an aqueous suspension suitablefor oral adminstration.

The extracts of Avena are normally administered orally in a dosagecorresponding to the extract of about 1 to 1.5 grams of the whole greenplant per day. This dosage is preferably divided, e.g. into quarterswhich are separately administered as in the trial described above. Anysuitable dosage form, e.g. any one of the compositions described in theExamples above, may be used.

I claim:

1. A method of reducing dependence on tobacco which comprisesadministering orally to a person dependent thereon a sufficient amountof a tobacco dependence reducing substance extracted from a whole maturegreen Avena plant selected from the group consisting of Avena sativa,Avena steritis, Avena strigosa and Avena fatua to reduce saiddependence, the tobacco dependence reducing substance corresponding tothat obtained by solvent extraction of said Avena plant with from about1 to 10 parts by volume of solvent per part by weight of plant, theextraction being carried out at from ambient temperature to 50C. andsaid solvent being selected from the group consisting of water, ethylalcohol, acetone, 21 chlorinated hydrocarbon, diethyl ether, hexane ormixtures thereofv 2. The method according to claim 1 wherein the tobaccodependence reducing substance is extracted from the Avena plant with asolvent selected from the group consisting of water, ethyl alcohol ormixtures thereof.

3. The method according to claim 1 wherein the amount of tobaccodependence reducing substance administered orally per day is equivalentto the aqueous alcoholic extract of about 1 to 1.5 grams of Avena plant.

4. The method according to claim 1 wherein the tobacco dependencereducing substance is obtained by extracting an Avena sativa plant withabout aqueous ethyl alcohol at substantially ambient temperature.

5. The method according to claim 1 wherein the tobacco dependencereducing substance is administered with water.

6. The method according to claim 1 wherein the tobacco dependencereducing substance is administered in association with apharmaceutically compatible carrier.

7. The method according to claim 1 wherein the Avena plant is Avenasativa, the cultivated oat plant.

8. A composition for oral administration to reduce dependence on tobaccowhich comprises a tobacco dependence reducing substance extracted from awhole the group consisting of water, ethyl alcohol, acetone, achlorinated hydrocarbon, diethyl ether, hexane or mixtures thereof.

9. The composition according to claim 8 in the form of a capsule ortablet.

10. The composition according to claim 8 in the form of a syrup orelixir.

2. The method according to claim 1 wherein the tobacco dependencereducing substance is extracted from the Avena plant with a solventselected from the group consisting of water, ethyl alcohol or mixturesthereof.
 3. The method according to claim 1 wherein the amount oftobacco dependence reducing substance administered orally per day isequivalent to the aqueous alcoholic extract of about 1 to 1.5 grams ofAvena plant.
 4. The method according to claim 1 wherein the tobaccodependence reducing substance is obtained by extracting an Avena sativaplant with about 90% aqueous ethyl alcohol at substantially ambienttemperature.
 5. The method according to claim 1 wherein the tobaccodependence reducing substance is administered with water.
 6. The methodaccording to claim 1 wherein the tobacco dependence reducing substanceis administered in association with a pharmaceutically compatiblecarrier.
 7. The method according to claim 1 wherein the Avena plant isAvena sativa, the cultivated oat plant.
 8. A composition for oraladministration to reduce dependence on tobacco which comprises a tobaccodependence reducing substance extracted from a whole mature green Avenaplant selected from the group consisting of Avena sativa, Avenasteritis, Avena strigosa and Avena fatua and a pharmaceuticallyacceptable carrier material, the tobacco dependence reducing substancecorresponding to that obtained by solvent extraction of said Avena plantwith from about 1 to 10 parts by volume of solvent per part by weight ofplant, the extraction being carried out at from ambient temperature to50*C. and said solvent being selected from the group consisting ofwater, ethyl alcohol, acetone, a chlorinated hydrocarbon, diethyl ether,hexane or mixtures thereof.
 9. The composition according to claim 8 inthe form of a capsule or tablet.
 10. The composition according to claim8 in the form of a syrup or elixir.